The present invention relates to readily absorbable enteral pharmaceutical formulations of pharmacologically active agents which are poorly absorbable per se, and to a method for preparing such formulations.
It is well known in the art that a number of pharmacologically active agents are absorbed in the gastrointestinal tract only to a low and unpredictable percent, or not at all. For some pharmacologically active agents, the poor enteral absorbability may be due to their insufficient solubility in water. Yet, pharmacologically active agents which are not satisfactorily enterally absorbable are also found amongst water soluble pharmacologically active agents.
In some cases, the absorbability of such unsufficiently enterally absorbable pharmacologically active ingredients can be improved by means of a technological treatment of the pharmacologically active agent, e.g., by means of micronization, formation of an adsorbate or adduct or addition of dissolving additives. Yet, the enterally applied dosage which is necessary to achieve a desired pharmacological effect, nearly always is substantially higher than the amount of the pharmacologically active agent which would be required in the case of a complete bioavailibility of this agent.
Yet, there is a need for pharmaceutical formulations which provide such per se poorly enterally absorbable pharmacologically active agents not only in an injectable formulation, but also in orally and/or rectally applyable formulations which provide a high degree of enteral absorption of these pharmacologically active agents.